Percutaneous absorption preparation for treating dementia comprising donepezil
Inventors
Jang, Sun-Woo • Shin, Chang-Yell • Kim, Jeong-Soo • Kim, Hae-Sun • Cha, Kwang-Ho • Kim, Hyun-Jung • Goto, Masaoki
Assignees
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Publication Number
US-11992562-B2
Publication Date
2024-05-28
Expiration Date
Abstract
A percutaneous absorption preparation is disclosed. The percutaneous absorption preparation contains donepezil for treatment of dementia, wherein the preparation includes: (a) donepezil or its pharmaceutically acceptable salt as active component, (b) propylene glycol monocaprylate as solubilizer, and (c) styrene-isoprene-styrene block copolymer (“SIS”) as adhesive. The percutaneous absorption preparation has low skin irritation and high skin penetration.
Core Innovation
The invention relates to a percutaneous absorption preparation for the treatment of dementia comprising a backing layer, a drug-containing layer, and a release liner. The drug-containing layer includes donepezil or a pharmaceutically acceptable salt thereof as an active component, propylene glycol monocaprylate as a solubilizer, a styrene-isoprene-styrene block copolymer as an adhesive, and a plasticizer.
The formulation specifies that the ratio of donepezil or the pharmaceutically acceptable salt thereof to the propylene glycol monocaprylate is not less than 1:1.5 by weight. The styrene-isoprene-styrene block copolymer is present at 10–70 wt% of the total weight of the drug-containing layer, and the plasticizer is selected from paraffin process oil, naphthalene process oil, aromatic process oil, olive oil, camellia oil, tall oil, castor oil, isopropyl myristate, hexyl lauric acid, mineral oil, octyldodecyl myristate, propylene glycol, and combinations thereof.
A key aspect of the invention is the use of propylene glycol monocaprylate with the adhesive styrene-isoprene-styrene block copolymer in the layered patch structure to address physicochemical stability and skin performance. The disclosure emphasizes that donepezil crystal precipitation is avoided, and that the preparation provides low skin irritation and high skin penetration.
The invention is illustrated with comparative results against a marketed Exelon® patch, including in-vitro Franz diffusion cell evaluation and in-vivo rat pharmacokinetics and rabbit skin irritation evaluation. The results reported in the disclosure indicate superior skin penetration and tolerability relative to the marketed Exelon® patch, with attention to drug release profile and avoidance of donepezil crystal precipitation.
Claims Coverage
The independent claim defines a percutaneous absorption preparation for treating dementia using a three-layer structure and a specific drug-containing layer composition, with five inventive features. Only one independent claim is provided in the supplied claim text (clm-00001).
Layered percutaneous absorption patch structure for dementia treatment
A percutaneous absorption preparation for the treatment of dementia comprising a backing layer, a drug-containing layer, and a release liner.
Drug-containing layer with donepezil, propylene glycol monocaprylate solubilizer, and SIS adhesive
The drug-containing layer comprises donepezil or a pharmaceutically acceptable salt thereof as an active component, propylene glycol monocaprylate as a solubilizer, a styrene-isoprene-styrene block copolymer as an adhesive, and a plasticizer.
Donepezil-to-propylene glycol monocaprylate weight ratio
A ratio of donepezil or the pharmaceutically acceptable salt thereof to the propylene glycol monocaprylate is not less than 1:1.5 by weight.
SIS adhesive amount in drug-containing layer
The styrene-isoprene-styrene block copolymer makes up 10–70 wt% of a total weight of the drug-containing layer.
Selected plasticizer group for drug-containing layer
The plasticizer is selected from the group consisting of paraffin process oil, naphthalene process oil, aromatic process oil, olive oil, camellia oil, tall oil, castor oil, isopropyl myristate, hexyl lauric acid, mineral oil, octyldodecyl myristate, propylene glycol, and a combination thereof.
Overall claim coverage centers on a dementia percutaneous absorption preparation with a backing layer, a drug-containing layer, and a release liner, where the drug-containing layer uses donepezil with propylene glycol monocaprylate as a solubilizer and a styrene-isoprene-styrene block copolymer as an adhesive. The claim further requires a minimum donepezil-to-solubilizer weight ratio, a defined SIS wt% range, and a plasticizer selected from a specified list.
Stated Advantages
Avoidance of donepezil crystal precipitation (improved physicochemical stability).
Low skin irritation.
High skin penetration.
Superior skin penetration and tolerability versus the marketed Exelon® patch.
Documented Applications
Percutaneous absorption treatment of dementia using a layered patch structure comprising a backing layer, a drug-containing layer, and a release liner.
Comparative evaluation versus a marketed Exelon® patch using in-vitro Franz diffusion cell studies, in-vivo rat pharmacokinetics, and rabbit skin irritation evaluation.
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